1,720,982 research outputs found
Interaction of difunctional aromatic platinum(II) complexes with the G-quadruplex structure of the telomeric sequence
No full textApplication of the anthraquinone drug rhein as an axial ligand in bifunctional Pt(IV) complexes to obtain antiproliferative agents against human glioblastoma cells
No full textOctahedral Pt(IV) prodrugs are an effective way to combine cisplatin-like moieties and a second drug to obtain selective and stimuli responsive bifunctional antiproliferative compounds. Recently, two bifunctional Pt(IV) complexes have shown interesting in vitro and in vivo effects in glioblastoma, the most aggressive primary brain tumor. An interesting observation indicates that 4,5-dihydroxy-9,10-dioxo-9,10-dihydroanthracene-2-carboxylic acid (rhein) can inhibit in vivo glioma tumor progression. Furthermore, a prodrug in which cisplatin was combined with two molecules of rhein showed a potency higher than that of cisplatin toward cisplatin-resistant lung carcinoma cells. However, the high lipophilicity of this type of complex affects their solubility and bioavailability. To overcome these limits, in the present work, three Pt (iv) derivatives were obtained by differently linking one molecule of rhein and one acetato ligand at the axial position to a cisplatin core. The complexes proved to be similar to or more potent than the parent cisplatin and rhein, and the reference drug temozolomide on two human glioblastoma cell lines (U87MG and T98G). They retained their activity under hypoxia and caused a significant reduction in the motility of both cell lines, which can be related to their ability to inhibit MMP2 and MMP9 matrix metalloproteinases. Finally, physicochemical and computational studies indicated that these Pt(IV) derivatives are more prone than rhein to cross the blood-brain barrier
Platinum Complexes With Substituted Phosphines: Synthesis, Characterization, And Antiproliferative Activity
No full textAssessment of the in vivo antiproliferative activity of a novel platinum nanoparticulate pharmacophore
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Biological Activity of Enantiomeric Complexes [PtCl2L2] (L2 = Aromatic Bisphosphanes and Aromatic Diamines)
No full textStudy of the synthesis, antiproliferative properties, and interaction with DNA and polynucleotides of cisplatin-like Pt(II) complexes containing carcinogenic polyaromatic amines
No full textInhibition of STAT3 increases doxorubicin sensitivity in a human metastatic breast cancer cell line
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Relationship Among Potency (IC50), Reduction Potential (E°’) And Partition Coefficient (log Po/w) Of New Antitumour Pt(IV) Complexes
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